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Synthesis and investigation on antidiabetic activity of 4-(1-aryl-3-oxo-5-phenylpentylamino) benzenesulfonamide / 药学学报
Acta Pharmaceutica Sinica ; (12): 66-71, 2010.
Artículo en Chino | WPRIM | ID: wpr-250618
ABSTRACT
Searching for new antidiabetic lead compound, 4-(1-aryl-3-oxo-5-phenylpentylamino) benzenesulfonamides were designed and synthesized directly by three component one-pot condensation of 4-phenyl-2-butanone and sulfanilamide with some aromatic aldehydes at an yield of 23%-97%. The chemical structures of the twelve new Mannich bases were confirmed by 1H NMR, 13C NMR, FTIR, ESI-MS and HR-MS. The screening results of antidiabetic activity indicated that most of these title compounds possess alpha-glucosidase inhibitory activity, among which compound le is the strongest one. And compound 11 possesses good peroxisome proliferator-activated receptor response element (PPRE) agonist activity. The structure-activity relationship of these new beta-amino ketones containing benzenesulfonamide unit was also discussed preliminarily.
Asunto(s)
Texto completo: Disponible Índice: WPRIM (Pacífico Occidental) Asunto principal: Farmacología / Relación Estructura-Actividad / Sulfanilamidas / Sulfonamidas / Diseño de Fármacos / Química / Receptores Activados del Proliferador del Peroxisoma / Alfa-Glucosidasas / Inhibidores de Glicósido Hidrolasas / Hipoglucemiantes Idioma: Chino Revista: Acta Pharmaceutica Sinica Año: 2010 Tipo del documento: Artículo

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Texto completo: Disponible Índice: WPRIM (Pacífico Occidental) Asunto principal: Farmacología / Relación Estructura-Actividad / Sulfanilamidas / Sulfonamidas / Diseño de Fármacos / Química / Receptores Activados del Proliferador del Peroxisoma / Alfa-Glucosidasas / Inhibidores de Glicósido Hidrolasas / Hipoglucemiantes Idioma: Chino Revista: Acta Pharmaceutica Sinica Año: 2010 Tipo del documento: Artículo